The metabolic fate of 11-bromo[15-3H]vincamine in man
| Autor: | L. F. Chasseaud, A. Darragh, S. R. Biggs, B. C. Mayo, D. R. Hawkins, F. C. Leaf |
|---|---|
| Rok vydání: | 1985 |
| Předmět: |
Adult
medicine.medical_specialty Chromatography Gas Chemical Phenomena Vincamine Urine Pharmacology Gas Chromatography-Mass Spectrometry Single oral dose Feces Pharmacokinetics Oral administration Internal medicine medicine Humans Pharmacology (medical) Vinca Alkaloids Biotransformation Chromatography High Pressure Liquid Chemistry Hydrolysis Stereoisomerism Metabolism Human physiology Endocrinology medicine.drug |
| Zdroj: | European journal of drug metabolism and pharmacokinetics. 10(3) |
| ISSN: | 0378-7966 |
| Popis: | During 5 days following a single oral dose of 3H-11-bromovincamine (40 mg) to two human subjects, means of 55% and 27% of the 3H dose were excreted in the urine and faeces respectively, mainly within 24 and 48 h. Mean plasma concentrations of 3H reached a peak (1900 ng equiv./ml) at 1 h after dosing and declined biphasically with half-lives of 5 h and 11 h which were similar to half-lives for urinary excretion of 3H. Parent drug and 11-bromovincaminic acid were the major dose-related components in plasma at 1.5 and 3 h. Mean plasma concentrations of 11-bromovincamine reached a peak (620 ng/ml) at 0.75 h and declined biphasically with half-lives of about 1 h and 5 h. The major urinary metabolite was 11-bromovincaminic acid (31% dose). Also present in urine were 11-bromovincamine (3%), 11-bromoapovincamine (1%) and 2 unknown metabolites (9% and 6%). Similar metabolites were detected in faecal extracts. If inadequately stored in biological samples, 11-bromovincamine could be hydrolysed to 11-bromovincaminic acid and be epimerised to 11-bromo-epivincamine. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full text from SpringerLink